Expertise

We design and synthesize bifunctional molecules (i.e., MTDLs, hybrids, conjugates, co-drugs and PROTACs) using up-to-date synthetic techniques and facilities. We develop appropriate rational design strategies based on modular protocols and “linker” chemistry to combine two starting bioactive entities into the desired bifunctional tools. In doing so, we exploit efficient, green and sustainable synthetic strategies.

Polypharmacology is the design or use of pharmaceutical agents that act on multiple targets or disease pathways. A polypharmacology approach can be achieved by multiple drugs binding to multiple targets: (1) drug cocktail (2) fix-dose combination or (3) one drug binding to multiple targets, i.e. MTDLs.
Together with Professor C. Melchiorre, we coined the term multi-target-directed ligands (MTDLs), which “more completely describes those compounds that are effective in treating complex diseases because of their ability to interact with the multiple targets thought to be responsible for the disease pathogenesis” (DOI: 10.1021/jm7009364).

The development of MTDLs is a paradigm shift beyond the "one drug, one target, one disease" strategy, inspired by the need to find a successful therapy for the treatment of complex, multifactorial diseases and pathologies with drug resistance issues (e.g. neurodegenerative and neglected tropical diseases).